Further studies on the neuroleptic profile of manassantin A

Rao, Koppaka V.; Puri, V.N.; El-Sawaf, H. A.

doi:10.1016/0014-2999(90)90177-8

Cited by 6 publications

(2 citation statements)

References 11 publications

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“…Previously reported activities of manassantins A and B include a tranquilizer-like activity in mice (manassantin A) [31,32], inhibition of NFκB activation (manassantins A and B) [33,34], inhibition of human acyl-CoA: cholesterol acyltransferase-1 and -2 (manassantins A and B) [35], inhibition of PMA-induced cell aggregation (manassantins A and B) [36], and inhibition of HIF-1 activation (manassantin B) [13]. Most of these activities that have been demonstrated in either cell-based or enzyme-based assays require manassantin concentrations that are in the micromolar range.…”

Section: Effects Of S Cernuus Lignans On Mitochondrial Respirationmentioning

confidence: 99%

Saururus cernuus lignans—Potent small molecule inhibitors of hypoxia-inducible factor-1

Hossain

Kim

Baerson

et al. 2005

Biochemical and Biophysical Research Communications

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Hypoxia-inducible factor-1 (HIF-1) represents an important tumor-selective therapeutic target for solid tumors. In search of novel small molecule HIF-1 inhibitors, 5400 natural product-rich extracts from plants, marine organisms, and microbes were examined for HIF-1 inhibitory activities using a cell-based reporter assay. Bioassay-guided fractionation and isolation, followed by structure elucidation, yielded three potent natural product-derived HIF-1 inhibitors and two structurally related inactive compounds. In a T47D cell-based reporter assay, manassantin B 1 , manassantin A, and 4-O-methylsaucerneol inhibited hypoxia-induced HIF-1 activation with IC 50 values of 3, 3, and 20 nM, respectively. All three compounds are relatively hypoxia-specific inhibitors of HIF-1 activation, in comparison to other stimuli. The hypoxic induction of HIF-1 target genes CDKN1A, VEGF and GLUT-1 were also inhibited. These compounds inhibit HIF-1 by blocking hypoxia-induced nuclear HIF-1α protein accumulation without affecting HIF-1α mRNA levels. In addition, preliminary structure-activity studies suggest specific structural requirements for this class of HIF-1 inhibitors.

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Section: Effects Of S Cernuus Lignans On Mitochondrial Respirationmentioning

confidence: 99%

Saururus cernuus lignans—Potent small molecule inhibitors of hypoxia-inducible factor-1

Hossain

Kim

Baerson

et al. 2005

Biochemical and Biophysical Research Communications

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“…7 Manassantin A has also been associated with selective neuroleptic activity. 8 In their intial report, Rao and Alvarez 1a revealed the gross structure and only partial relative configuration of 1 and 2. They coined the name manassantin from the Sanskrit words "manas" or mind and "santi" or peace (i.e., peace of mind).…”

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confidence: 95%

Total Synthesis and Stereochemical Confirmation of Manassantin A, B, and B₁

2006

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Manassantin A and B fromSaururus chinensisinhibiting cellular melanin production

Seo¹,

Lee²,

Chung³

et al. 2009

Phytotherapy Research

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Hyperpigmentation disorders such as freckles and senile lentigines in the skin are associated with abnormal accumulation of melanin pigments. In this study, two lignan constituents were isolated from Saururus chinensis Baill (Saururaceae) as inhibitors of cellular melanin production by bioassay-guided fractionations. The active constituents were manassantin A and B that dose-dependently inhibited melanin production in alpha-melanocyte stimulating hormone (alpha-MSH)-activated melanoma B16 cells with IC(50) values of 13 nm and 8 nm, respectively. Arbutin as a positive control exhibited an IC(50) value of 96 microm on alpha-MSH-induced melanin production. Further, manassantin A inhibited forskolin- or 3-isobutyl-1-methylxanthine (IBMX)-induced melanin production with IC(50) values of 14 nm or 12 nm, respectively. Manassantin A decreased cellular amounts of IBMX-inducible tyrosinase protein but could not affect the catalytic activity of cell-free tyrosinase, a key enzyme in the biosynthetic pathway of melanin pigments. Finally, this study could provide a pharmacological potential of S. chinensis in hyperpigmentation disorders.

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Further studies on the neuroleptic profile of manassantin A

Cited by 6 publications

References 11 publications

Saururus cernuus lignans—Potent small molecule inhibitors of hypoxia-inducible factor-1

Saururus cernuus lignans—Potent small molecule inhibitors of hypoxia-inducible factor-1

Total Synthesis and Stereochemical Confirmation of Manassantin A, B, and B₁

Manassantin A and B fromSaururus chinensisinhibiting cellular melanin production

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Further studies on the neuroleptic profile of manassantin A

Cited by 6 publications

References 11 publications

Saururus cernuus lignans—Potent small molecule inhibitors of hypoxia-inducible factor-1

Saururus cernuus lignans—Potent small molecule inhibitors of hypoxia-inducible factor-1

Total Synthesis and Stereochemical Confirmation of Manassantin A, B, and B1

Manassantin A and B fromSaururus chinensisinhibiting cellular melanin production

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Total Synthesis and Stereochemical Confirmation of Manassantin A, B, and B₁